RU2710549C2 - Производное пиразола, пригодное в качестве ингибитора рi3к - Google Patents

Производное пиразола, пригодное в качестве ингибитора рi3к Download PDF

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Publication number
RU2710549C2
RU2710549C2 RU2017134110A RU2017134110A RU2710549C2 RU 2710549 C2 RU2710549 C2 RU 2710549C2 RU 2017134110 A RU2017134110 A RU 2017134110A RU 2017134110 A RU2017134110 A RU 2017134110A RU 2710549 C2 RU2710549 C2 RU 2710549C2
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Russia
Prior art keywords
compound
morpholin
methyl
mmol
pyrazol
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RU2017134110A
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English (en)
Russian (ru)
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RU2017134110A3 (ja
RU2017134110A (ru
Inventor
Кирандип Каур САМБИ
Йогеш Бабан СУРАСЕ
Сагар Рамдас АМАЛЬ
Суреш Кумар ГОРЛА
Приайанка ПАТЕЛ
Ашвани Кумар ВЕРМА
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Дайити Санкио Компани, Лимитед
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
RU2017134110A 2015-03-30 2016-03-29 Производное пиразола, пригодное в качестве ингибитора рi3к RU2710549C2 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
IN878DE2015 2015-03-30
IN878/DEL/2015 2015-03-30
PCT/IB2016/051762 WO2016157074A1 (en) 2015-03-30 2016-03-29 6-morpholinyl-2-pyrazolyl-9h-purine derivatives and their use as pi3k inhibitors

Publications (3)

Publication Number Publication Date
RU2017134110A RU2017134110A (ru) 2019-04-03
RU2017134110A3 RU2017134110A3 (ja) 2019-06-11
RU2710549C2 true RU2710549C2 (ru) 2019-12-27

Family

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RU2017134110A RU2710549C2 (ru) 2015-03-30 2016-03-29 Производное пиразола, пригодное в качестве ингибитора рi3к

Country Status (30)

Country Link
US (1) US10174035B2 (ja)
EP (1) EP3277682B1 (ja)
JP (1) JP6669417B2 (ja)
KR (1) KR20170131444A (ja)
CN (1) CN107428756B (ja)
AU (1) AU2016242080B2 (ja)
BR (1) BR112017020818A2 (ja)
CA (1) CA2980517C (ja)
CO (1) CO2017011020A2 (ja)
CY (1) CY1122018T1 (ja)
DK (1) DK3277682T3 (ja)
ES (1) ES2733505T3 (ja)
HK (1) HK1250161B (ja)
HR (1) HRP20190998T1 (ja)
HU (1) HUE045192T2 (ja)
IL (1) IL254688B (ja)
LT (1) LT3277682T (ja)
MX (1) MX2017012390A (ja)
MY (1) MY185268A (ja)
PH (1) PH12017501750A1 (ja)
PL (1) PL3277682T3 (ja)
PT (1) PT3277682T (ja)
RS (1) RS59213B1 (ja)
RU (1) RU2710549C2 (ja)
SG (1) SG11201706509QA (ja)
SI (1) SI3277682T1 (ja)
TR (1) TR201910941T4 (ja)
TW (1) TWI689508B (ja)
WO (1) WO2016157074A1 (ja)
ZA (1) ZA201705530B (ja)

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TW201817731A (zh) * 2016-09-29 2018-05-16 日商第一三共股份有限公司 ［２－（１－甲基－１ｈ－吡唑－４－基）－６－（ 啉－４－基）－９ｈ－嘌呤－８－基］［４－（ 啉－４－基）哌啶－１－基］甲酮及其製藥上容許鹽之結晶
CN107163061A (zh) * 2017-04-14 2017-09-15 江西科技师范大学 含吡唑啉结构的噻吩并嘧啶类化合物的制备及应用
CN110963955A (zh) * 2018-09-30 2020-04-07 南京富润凯德生物医药有限公司 一种单氟代螺环化合物的合成方法及其中间体
CN111087336A (zh) * 2018-10-24 2020-05-01 南京富润凯德生物医药有限公司 一种双氟代螺环化合物的合成方法及其中间体
CN110577515B (zh) * 2019-09-02 2022-05-17 南通大学 一种4-(氮杂环丁烷-3-基)-1-甲基哌嗪-2-酮二盐酸盐的合成方法

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WO2010138589A1 (en) * 2009-05-27 2010-12-02 Genentech, Inc. Bicyclic pyrimidine pi3k inhibitor compounds selective for p110 delta, and methods of use
RU2437888C2 (ru) * 2006-04-26 2011-12-27 Дженентек, Инк. Ингибиторы фосфоинозитид-3-киназы и содержащие их фармацевтические композиции
RU2443706C2 (ru) * 2006-04-26 2012-02-27 Дженентек, Инк. Фармацевтические соединения

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CA2527079A1 (en) 2003-05-29 2005-01-06 Synta Pharmaceuticals, Corp. Heterocyclic compounds for preventing and treating disorders associated with excessive bone loss
GB2431156A (en) 2005-10-11 2007-04-18 Piramed Ltd 1-cyclyl-3-substituted- -benzenes and -azines as inhibitors of phosphatidylinositol 3-kinase
US20080233127A1 (en) 2007-03-21 2008-09-25 Wyeth Imidazolopyrimidine analogs and their use as pi3 kinase and mtor inhibitors
WO2009034386A1 (en) 2007-09-13 2009-03-19 Astrazeneca Ab Derivatives of adenine and 8-aza-adenine and uses thereof-796
RU2681081C2 (ru) 2007-10-05 2019-03-04 Верастэм, Инк. Пиримидинзамещенные производные пурина, фармацевтическая композиция на их основе, способ ингибирования протеинкиназ, способ лечения или профилактики заболеваний, чувствительных к ингибированию протеинкиназ, и способ лечения пролиферативных заболеваний
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RU2443706C2 (ru) * 2006-04-26 2012-02-27 Дженентек, Инк. Фармацевтические соединения
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Publication number Publication date
EP3277682A1 (en) 2018-02-07
AU2016242080A1 (en) 2017-08-24
JP2018510146A (ja) 2018-04-12
ES2733505T3 (es) 2019-11-29
SG11201706509QA (en) 2017-09-28
CA2980517C (en) 2020-02-25
WO2016157074A1 (en) 2016-10-06
LT3277682T (lt) 2019-06-25
PH12017501750A1 (en) 2018-04-02
CY1122018T1 (el) 2020-10-14
RU2017134110A3 (ja) 2019-06-11
CN107428756A (zh) 2017-12-01
TW201643162A (zh) 2016-12-16
EP3277682B1 (en) 2019-04-24
IL254688A0 (en) 2017-11-30
MY185268A (en) 2021-04-30
TWI689508B (zh) 2020-04-01
MX2017012390A (es) 2018-01-26
RS59213B1 (sr) 2019-10-31
CO2017011020A2 (es) 2018-01-16
HRP20190998T1 (hr) 2019-10-18
US10174035B2 (en) 2019-01-08
PL3277682T3 (pl) 2019-09-30
RU2017134110A (ru) 2019-04-03
JP6669417B2 (ja) 2020-03-18
PT3277682T (pt) 2019-07-09
IL254688B (en) 2021-03-25
TR201910941T4 (tr) 2019-08-21
CA2980517A1 (en) 2016-10-06
CN107428756B (zh) 2019-07-23
DK3277682T3 (da) 2019-07-29
ZA201705530B (en) 2018-05-30
HUE045192T2 (hu) 2019-12-30
KR20170131444A (ko) 2017-11-29
US20180072732A1 (en) 2018-03-15
AU2016242080B2 (en) 2019-09-19
BR112017020818A2 (pt) 2018-07-03
SI3277682T1 (sl) 2019-06-28
HK1250161B (zh) 2020-05-15

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